The weight control product of the present invention is designed to promote weight loss as a component of a weight control program for individuals who are overweight and desire to lose body fat and/or reduce their plasma lipid levels. The product according to the invention is consumed as a nutritional supplement and is preferably incorporated into a multi-disciplinary nutritional program such as the American Heart Association Step One Diet.
Numerous weight control products are known in the literature. One example of a weight control product is taught in U.S. Pat. No. 4,959,227 to Amer wherein the product has a reduced lactose content and contains dietary fiber. In similar fashion, U.S. Pat. No. 5,104,676 to Mahmoud et al. discloses a weight loss product that utilizes a particular blend of soluble, insoluble, fermentable and non-fermentable fibers. Commercially available weight control products include Ultra-Slim Fast.RTM. which is distributed by Slim Fast Foods, a division of Thompson Medical Company, Inc. New York, N.Y. and OpitiTrim.RTM. which is available from the Clinical Products Division of Sandoz Nutrition Corp., Minneapolis, Minn. In addition, literally hundreds of chemical entities have been suggested as weight loss products, however, none of the prior art has suggested or disclosed the combined use of a guggul extract with a blend of phosphate salts to result in a composition that is highly effective in reducing the weight of a mammal through primarily a loss of body fat while at the same time dramatically decreasing the blood plasma lipid levels of the individual, enhancing the mood states and increasing vigor.
A compound known as Z-guggulsterone has been identified as having the following structural formula: ##STR1## The E-stereoisomer has also been identified and these ketones are known hypolipemic and antiplatelet aggregation agents. A process for the preparation of pharmacologically active synthetic Z and E stereoisomeric mixture of guggulsterones is disclosed in EP0447,706 to Hamied. These compounds have also been isolated from the exudate of a plant known as Commiphora mukul (Hook, ex stocks) Engl. (syn. Balsamodendron mukul Hook) which is a small tree of the Burseraceae family, endemic in the Indian peninsula. If the trunk is etched, the plant emits a yellowish gummy exudate, which coagulates rapidly in the form of stalactites having a balsamic smell. In the ancient Sanskrit, this gum resin is called guggulu and is a product which is still used in Indian popular medicine for the treatment of obesity and some arthritic diseases. Recently, a lipophilic extract has been prepared from this resin, this extract contains many classes of compounds, among which lignans, terpenes and some keto-steroids, named Guggulsterones. Hypolipidemic and platelet aggregation inhibiting activities are described for this lipophilic extract, which is normally obtained by simple resin extraction with ethyl acetate, or for Guggulsterone-Z and Guggulsterone-E, whose components in the extract are normally titrated.
By studying this resin, it has unexpectedly been found that the lipophilic extract with ethyl acetate or some fractions obtained from it when combined with a mixture of phosphate salts demonstrates outstanding weight loss, fat loss, mood elevating and hyperlipidemic properties. Further, the synergistic action of the extract and mixture of phosphate salts has demonstrated efficacy in elevating the vigor of individuals consuming it.
The extract is prepared by etching Commiphora mukul bark and obtaining the resin from it. The resin is then dried, ground and subjected to extensive extraction with ethyl acetate. The collected extracts may then be treated with charcoal. After charcoal separation, the colorless solution is concentrated to obtain a thick paste, which is recovered with ethanol, and, after filtrating the insoluble matter, concentrated with complete solvent removal.
Indian Complete Specification No. 166998 discloses a method for the manufacture of a pharmaceutical composition of guggulipid in solid dosage form. The guggulipid is disclosed as being mixed with excipients and granulating agents and thereafter pressed into the solid dosage form. This reference also states that in biological tests in rats and mice with the dosage form, pharmacological activities such as hypolipedemic, antiobesity and hypocholesterolemic were observed.
U.S. Pat. No. 5,273,747 to Bombardellie et al. discloses that the Commiphora mukul lipophilic extracts have therapeutic applications in the treatment of inflammations of the skin and external mucosa and in the symptomatic treatment of benign prosthetic hypertrophy and in the treatment of acne.
A study of the effects of guggulsterone on hypolipidemia is reported in an article by Beg, et al. Indian-J-Physiol-Pharmacol. 1996 July; 40 (3): 237-40. This article reports that the administration of guggulsterone in daily divided doses of 75 mg for a period of eight (8) weeks together with supportive measures like a high protein diet, diuretics and hematinics resulted in a significant reduction of total serum lipid and total serum cholesterol. No mention is made of weight loss in this publication, nor is it suggested to combine the guggulsterone with a mixture of phosphate salts to produce synergistic effects.
In an article published by Tripathia, et al. entitled Thyroid Stimulatory Action of Z-Guggulsterone: Mechanism of Action. Planta-Med., 1988 August; 54(4): 271-7 the authors disclose that guggulsterone is effective in stimulating the activity of the thyroid gland in rats. The guggulsterone used in this study is disclosed as being a ketosteroid isolated from the oleoresin of the dry exudate of Commiphora mukul. The compound was shown to counteract the thyroid suppressant activity of a known thyroid inhibitor (carbimazole).
Agarwal, et al. investigated the use of gugulipid as a hyperlipidemic agent. Indian-J-Med-res. 1986 December; 84:626-34. In similar fashion, guggulsterones have also been found to be very effective in reducing total cholesterol levels and LDL levels. Nityanand et al. report in "Clinical Trials With Gugulipid, A New Hyperlipidaemic Agent" J-Assoc-Physicians-India, 1989 May; 37(5): 323-8, a multi-center clinical trial with 205 patients over a twelve (12) week period. A gugulipid dose of 500 mg twice daily after eight (8) weeks showed a significant lowering in the serum cholesterol (average 23.6%) and serum triglycerides (average 22.6%). The study also used colfibrate as a comparative. The gugulipid average fall in serum cholesterol and triglycerides was 11 and 16.8% respectively and with colfibrate 10 and 21.6% respectively. The lipid lowering effect of both drugs became evident three (3) to four (4) weeks after starting the drugs. Nityanand et al. also reported that hypocholesterolemic patients responded better to gugulipid therapy than hypertriglyceridemic patients who responded better to colfibrate therapy. HDL-cholesterol was increased in sixty percent (60%) of the cases who responded to the gugulipid therapy, in contrast colfibrate had no effect on HDL-cholesterol.
U.S. Pat. No. 5,690,948 to McCook et al. discloses gugulipid (a lipophilic ethyl acetate extract from C. Mukul or C. Wightii) and an alcoholic fraction of gugulipid as an antisebum and/or antioxidant for skin care compositions. This patent does not suggest or disclose the combination of gugulipid with a mixture of phosphate salts to create a weight control product. One important aspect of the inventive weight control product is the synergistic effect that is obtained by combining the guggul extract with a sufficient amount of phosphate salts.
A number of studies have recently investigated the effect of calcium phosphate, potassium phosphate and sodium phosphate to increase the basal metabolic rate (BMR) and increase thyroid activity. For example, see Nazar et al. "Phosphate Supplementation Prevents A Decrease In Triiodothyronine And Increases Resting Metabolic Rate During Low Energy Diet" J-Physiol-Pharmacol. 1996 June; 47(2): 373-83. In the Nazer et al. study thirty (30) over-weight women participated in an eight (8) week slimming program consisting of a self controlled, low energy diet (4.2 MJ per day) supplemented with highly viscous fibers and mineral tablets containing calcium, potassium and sodium phosphates. This was a double blind, cross-over study. During periods of phosphate supplementation, the resting metabolic rate (RMR) increased by approximately twelve percent (12%) (p&lt;0.05) in group one and nineteen percent (19%) (p&lt;0.05) in group two. The study reported that there were no differences between groups in the plasma insulins catecholamine, growth hormone, cortisol and testosterone levels. It was also reported that phosphate supplementation did not effect plasma lipids or blood glucose concentration.
Kaciuba et al. reported in "Effective Phosphate Supplementation On Metabolic and Neuroendocrine Responses To Exercise And Oral Glucose Load In Obese Women During Weight Reduction" J-Physiol-Pharmacol 1993 December; 44(4): 425-40; a study wherein 36 obese women participated in a four (4) week weight reducing program. All of them complied with a low fat diet of approximately one thousand (1000) calories per day with high viscous fiber capsules as a basic supplement. Group One (n=18) received mineral tablets containing mainly calcium and potassium phosphates while the remaining subjects (Group Two) were given a placebo tablet. This study reports that weight loss during energy restriction was not affected by phosphate supplementation, however, the phosphates caused a significant increase (p&lt;0.05) in the resting metabolic rate.
For every form of life, phosphates play an essential role in all energy transfer processes such as metabolism, photosynthesis, nerve function, and muscle action. The nucleic acids, which among other things make up the hereditary material (the chromosomes) are phosphates, as are a number of coenzymes. The phosphates are based on phosphorus atoms tetrahedrally surrounded by oxygen atoms, with the lowest member of the series being the simple PO.sub.4.sup.-3 anion (the orthophosphate ion). The phosphorus compound of major biological importance is adenosinetriphosphate (ATP), which is an ester of the salt, sodium tripolyphosphate, widely employed in detergents and water softening compounds. Practically every reaction in metabolism and photosynthesis involves hydrolysis of this tripolyphosphate to its pyrophosphate derivative, called adenosinediphosphate (ADP).
Phosphates are used as dietary supplements for patients who are unable to get enough phosphorus in their regular diet, usually because of certain illnesses or diseases. Injectable phosphates are administered only by or under the supervision of a health care professional. Various forms of phosphates are available without a prescription. Often tablets and powders are dissolved in a liquid prior to consumption. This is done to avoid or lessen possible side effects which include diarrhea, nausea, vomiting and stomach pain.
While the prior art discloses the use of guggulsterones to reduce blood plasma lipid content and the use of phosphates to decrease triiodothyronine and increase resting metabolic rate, there is no suggestion or disclosure of combining these materials to achieve a synergistic effect in weight control and the surprising benefits of enhanced mood states and increased vigor.